Green synthesis method of 2-trifluoromethylindole

Abstract

The invention discloses a green synthesis method of 2-trifluoromethylindole, which comprises the following steps: (1) mixing EDC, triphenylphosphine, triethylamine, trifluoroacetic acid, o-toluidine, a sodium bromide solution and alkali to obtain a reaction solution A; (2) conducting heating, conducting irradiating with an ultraviolet lamp, and adding a sodium hypochlorite solution to obtain a reaction solution B; (3) refluxing the reaction liquid B, conducting cooling and splitting phases to obtain a water phase I and an organic phase I; (4) extracting the water phase I with EDC to obtain an extracting solution; (5) filtering the organic phase I, and washing a filter cake with EDC to obtain a washing solution; (6) mixing the extracting solution, the filtrate and the washing solution, and conducting washing and drying to obtain a mixed solution; (7) conducting desolventizing and distilling to obtain a white intermediate; (8) dissolving the intermediate into a reaction solution C, then enabling a formed solution to flow through a magnesium fixed bed, conducting cooling after reaction, and adding an ammonium chloride aqueous solution for hydrolysis and phase separation to obtain a water phase II and an organic phase II; and (9) adding salt into the water phase II for saturation, conducting extracting with an organic solvent, mixing the extract and the organic phase II, and conducting washing, drying, desolventizing and crystallizing to obtain the product.

Description

technical field

[0001] The invention relates to the field of compound synthesis, in particular to a green synthesis method of 2-trifluoromethyl indole; the synthesis method of the invention has the characteristics of high efficiency and low pollution, and is a green and environment-friendly synthesis process. Background technique

[0002] Indole derivatives such as tryptophan and its metabolites, indole alkaloids, etc. are widely distributed in nature, and they provide the main framework of compounds for the discovery and development of new biologically active compounds. Studies have found that indole derivatives have various important biological activities, and the indole molecular skeleton plays an important role in the synthesis of various new drugs. For example, the indole acetic acid drug indomethacin is a non-steroidal anti-inflammatory drug, which has anti-inflammatory, antipyretic and analgesic effects; cyclomazindole and clomizindole can suppress appetite and reduce...